4-(2-乙酰氧基苯甲酰氨基) 丁酰胺衍生物的设计、合成及初步活性研究

Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives

摘要:
为了寻找新型γ-氨基丁酸 (γ-aminobutyric acid, GABA) 类抗癫痫药物, 以抑制性神经递质γ-氨基丁酸受体 (GABA_R) 为作用靶点, 以GABA为原料设计合成了一类全新结构类型的4-(2-乙酰氧基苯甲酰氨基) 丁酰胺类化合物 (5a～5l), 通过IR、¹H MNR、EI-MS及元素分析确证了目标化合物的结构。初步药理活性评价结果表明, 目标化合物具有良好抗癫痫活性, 值得进一步研究, 在此基础上, 初步讨论了该类化合物的构效关系。

Abstract:
To explore new agents of γ-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a−5l) were synthesized from GABA as starting material, and their structures were confirmed with IR, ¹H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.